专利号:US-11649285-B2 优先权日:2016-08-03 标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy 发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN 权利人:BIO TECHNE CORP 摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.
专利号:US-10370455-B2 优先权日:2014-12-05 标题 :Identification of VSIG8 as the putative VISTA receptor (V-R) and use thereof to produce VISTA/VSIG8 agonists and antagonists 发明人:MOLLOY MICHAEL; GUO YALIN; ROTHSTEIN JAY; ROSENZWEIG MICHAEL 权利人:IMMUNEXT INC 摘要:The receptor for VISTA is identified (VSIG8) as well as the use of this receptor in the identification or synthesis of agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG8 and/or VISTA and/or the VSIG8/VISTA binding interaction. These antagonists may be used to suppress VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.
专利号:US-2018371021-A1 优先权日:2017-05-11 标 题 :Peptidomimetic macrocycles and uses thereof 发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:US-2024066133-A1 优先权日:2020-03-06 标 题 :Therapeutic agents and conjugates thereof 发明人:SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO 权利人:BEIJING XUANYI PHARMASCIENCES CO LTD 摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.
1: Bitzer M, Horger M, Giannini EG, Ganten TM, Wörns MA, Siveke JT, Dollinger MM, Gerken G, Scheulen ME, Wege H, Zagonel V, Cillo U, Trevisani F, Santoro A, Montesarchio V, Malek NP, Holzapfel J, Herz T, Ammendola AS, Pegoraro S, Hauns B, Mais A, Lauer UM, Henning SW, Hentsch B. Resminostat plus sorafenib as second-line therapy of advanced hepatocellular carcinoma - The SHELTER study. J Hepatol. 2016 Aug;65(2):280-8. doi: 10.1016/j.jhep.2016.02.043. Epub 2016 Mar 4. 5(5-6):196-208. doi: 10.18632/oncoscience.420. 3: Walewski J, Paszkiewicz-Kozik E, Borsaru G, Hellmann A, Janikova A, Warszewska A, Mais A, Ammendola A, Herz T, Krauss B, Henning SW. Resminostat in patients with relapsed or refractory Hodgkin lymphoma: results of the phase II SAPHIRE study. Leuk Lymphoma. 2019 Mar;60(3):675-684. doi: 10.1080/10428194.2018.1492122. Epub 2018 Aug 30. 10(6):2088-2099. doi: 10.1002/cam4.3813. Epub 2021 Feb 26. 5: Soukupova J, Bertran E, Peñuelas-Haro I, Urdiroz-Urricelqui U, Borgman M, Kohlhof H, Fabregat I. Resminostat induces changes in epithelial plasticity of hepatocellular carcinoma cells and sensitizes them to sorafenib-induced apoptosis. Oncotarget. 2017 Nov 30;8(66):110367-110379. doi: 10.18632/oncotarget.22775.
合成参考文献
参考文献:10.1002/hed.24699 摘要:Enzenhofer E, Kadletz L, Stanisz I, Kotowski U, Seemann R, Schmid R, Thurnher D, Heiduschka G. Effect of the histone deacetylase inhibitor resminostat on head and neck squamous cell carcinoma cell lines. Head Neck. 2017 May;39(5):900–7. doi: 10.1002/hed.24699.